CA3149482A1 - Derives de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composes apparentes utilises en tant qu'agonistes de sting (stimulateur des genes de l'interferon) pour le traitement du cancer - Google Patents

Derives de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composes apparentes utilises en tant qu'agonistes de sting (stimulateur des genes de l'interferon) pour le traitement du cancer Download PDF

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CA3149482A1
CA3149482A1 CA3149482A CA3149482A CA3149482A1 CA 3149482 A1 CA3149482 A1 CA 3149482A1 CA 3149482 A CA3149482 A CA 3149482A CA 3149482 A CA3149482 A CA 3149482A CA 3149482 A1 CA3149482 A1 CA 3149482A1
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alkyl
optionally substituted
alkoxy
amino
independently
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Jeremy R. Duvall
Keith W. Bentley
Brian D. Jones
Eugene W. Kelleher
Soumya S. RAY
Joshua D. Thomas
Dorin Toader
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Mersana Therapeutics Inc
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Mersana Therapeutics Inc
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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Abstract

La présente invention concerne des composés de formule (IA') en tant qu'agonistes de STING (stimulateur des gènes de l'interféron) destinés à être utilisés dans le traitement, par exemple, du cancer, de l'obésité, de lésions hépatiques, du métabolisme des glucides et des lipides et d'infections virales. La présente invention concerne la synthèse et la caractérisation de composés donnés à titre d'exemple, ainsi que des données pharmacologiques de ceux-ci (par exemple, pages 128 à 286 ; exemples 1 à 54 ; tableaux 1, 2a, 2b et 3). Un exemple de composés est par exemple, exemple 1 : (E)-N-(5-carbamoyl- l-(4-(5-carbamoyl-2-(4-éthyl-2-méthyloxazole-5-carboxamido)-7- (3-hydroxypropoxy)-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-7- méthoxy-1H-benzo[d]imidazol-2-yl)-4-éthyl-2-méthyloxazote-5- carboxamide (composé 9).
CA3149482A 2019-08-02 2020-07-31 Derives de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composes apparentes utilises en tant qu'agonistes de sting (stimulateur des genes de l'interferon) pour le traitement du cancer Pending CA3149482A1 (fr)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201962882081P 2019-08-02 2019-08-02
US62/882,081 2019-08-02
US201962944643P 2019-12-06 2019-12-06
US62/944,643 2019-12-06
US202062982935P 2020-02-28 2020-02-28
US62/982,935 2020-02-28
PCT/US2020/044538 WO2021026009A1 (fr) 2019-08-02 2020-07-31 Dérivés de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composés apparentés utilisés en tant qu'agonistes de sting (stimulateur des gènes de l'interféron) pour le traitement du cancer

Publications (1)

Publication Number Publication Date
CA3149482A1 true CA3149482A1 (fr) 2021-02-11

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CA3149482A Pending CA3149482A1 (fr) 2019-08-02 2020-07-31 Derives de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composes apparentes utilises en tant qu'agonistes de sting (stimulateur des genes de l'interferon) pour le traitement du cancer

Country Status (13)

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US (3) US11155567B2 (fr)
EP (1) EP4007758A1 (fr)
JP (1) JP7843695B2 (fr)
KR (1) KR20220056176A (fr)
CN (1) CN114585623A (fr)
AU (1) AU2020324388A1 (fr)
BR (1) BR112022001931A2 (fr)
CA (1) CA3149482A1 (fr)
IL (1) IL290212A (fr)
MX (2) MX2022001407A (fr)
TW (1) TW202120500A (fr)
WO (1) WO2021026009A1 (fr)
ZA (1) ZA202201505B (fr)

Cited By (1)

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Publication number Priority date Publication date Assignee Title
CN114948955A (zh) * 2022-06-06 2022-08-30 中国科学技术大学 靶向环鸟苷酸-腺苷酸合成酶的小分子共价抑制剂及其用途

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KR102726248B1 (ko) 2016-07-07 2024-11-05 더 보드 어브 트러스티스 어브 더 리랜드 스탠포드 주니어 유니버시티 항체-애쥬번트 접합체
MX2019011655A (es) 2017-03-29 2019-12-19 Legochem Biosciences Inc Profarmaco de dimero de pirrolobenzodiazepina y compuesto conjugado ligando-conector de este.
EP3919488B1 (fr) * 2019-01-31 2025-08-27 Hitgen Inc. Immunomodulateur
AU2020241686A1 (en) 2019-03-15 2021-11-04 Bolt Biotherapeutics, Inc. Immunoconjugates targeting HER2
CA3149482A1 (fr) 2019-08-02 2021-02-11 Mersana Therapeutics, Inc. Derives de bis-[n-((5-carbamoyl)-1h-benzo[d]imidazol-2-yl)-pyrazol-5-carboxamide] et composes apparentes utilises en tant qu'agonistes de sting (stimulateur des genes de l'interferon) pour le traitement du cancer
WO2021202984A1 (fr) 2020-04-02 2021-10-07 Mersana Therapeutics, Inc. Conjugués anticorps-médicament comprenant des agonistes de sting
WO2021206158A1 (fr) 2020-04-10 2021-10-14 小野薬品工業株式会社 Méthode de cancérothérapie
WO2022177307A1 (fr) * 2021-02-17 2022-08-25 한국화학연구원 Composition de stimulateur de gène d'interféron comprenant un dérivé de benzimidazole en tant que principe actif
CN116940574A (zh) * 2021-05-24 2023-10-24 福君基因公司 化合物及其作为疫苗佐剂的用途
EP4615853A2 (fr) * 2022-11-08 2025-09-17 LigaChem Biosciences Inc. Composés hétérocycliques utilisés comme agonistes de sting
WO2024174863A1 (fr) * 2023-02-22 2024-08-29 深圳众格生物科技有限公司 Agoniste de sting et procédé de préparation et utilisation médicale associés
WO2024182414A1 (fr) * 2023-02-27 2024-09-06 Biontech Us Inc. Agonistes de sting contenant des groupes fonctionnels hydrazide, hydrazine et acide hydroxamique
WO2024186626A1 (fr) * 2023-03-03 2024-09-12 Bolt Biotherapeutics, Inc. Immunoconjugués d'agonistes de sting aza-bicycliques et leurs utilisations
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